US2003191066A1PendingUtilityA1
Enone cancer therapeutics
Est. expiryMar 15, 2022(expired)· nominal 20-yr term from priority
A61K 31/56A61K 38/00C07K 5/0215
48
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Claims
Abstract
New enone derivatives and conjugates are described. These compounds can be used as cancer therapeutics.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A composition comprising an enone selected from the following group, stereoisomers thereof, and positional isomers thereof
wherein X is a nucleophilic atom selected from the group consisting of S, N, and O and R is selected from the group consisting of OCOCH=CHCH 3 , OCOCH 3 , OCOC 6 H 5 , OCONHCH 3 , estrogen, testosterone, sex hormone steroids, and therapeutically effective derivatives of sex hormone steroids.
2 . The enone of claim 1 comprising a derived glutathione adduct.
3 . The derived glutathione adduct of claim 2 wherein said glutathione adduct is produced by the action of glutathionyl transferase.
4 . The enone of claim 1 wherein the therapeutically effective derivatives of sex hormone steroids comprise estradiol conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
5 . The enone of claim 1 wherein the therapeutically effective derivatives of sex hormone steroids comprise testosterone conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
15 R′ = H, R =
16 R′ = H, R =
17 R = H, R′ =
18 R = H, R′ =
6 . The enone of claim 1 comprising a polymeric substance wherein the enone is bound to water-soluble copolymers.
7 . The enone of claim 6 wherein the water-soluble copolymers comprise N-(2-hydroxypropyl) methacrylamide copolymers.
8 . Cancer therapeutics comprising reactive compounds conjugated to tumor-targeting moieties, such cancer therapeutics being transformed intracellularly by the nucleophilic addition of reduced glutathione to then have their therapeutic effect by reacting, in turn, with cancer cell proteins or nucleic acids.
9 . A cancer therapeutic comprising an enone selected from following group, stereoisomers thereof, and positional isomers thereof
wherein X is a nucleophilic atom selected from the group consisting of S, N, and O and R is selected from the group consisting of OCOCH=CHCH 3 , OCOCH 3 , OCOC 6 H 5 , OCONHCH 3 , estrogen, testosterone, sex hormone steroids, and therapeutically effective derivatives of sex hormone steroids.
10 . The cancer therapeutic of claim 9 comprising a derived glutathione adduct.
11 . The derived glutathione adduct of claim 10 wherein said glutathione adduct is produced by the action of glutathionyl transferase.
12 . The cancer therapeutic of claim 9 wherein the therapeutically effective derivatives of sex hormone steroids comprise estradiol conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
13 . The cancer therapeutic of claim 9 wherein the therapeutically effective derivatives of sex hormone steroids comprise testosterone conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
15 R′ = H, R =
16 R′ = H, R =
17 R = H, R′ =
18 R = H, R′ =
14 . The cancer therapeutic of claim 9 comprising a polymeric substance wherein the cancer therapeutic is bound to water-soluble copolymers.
15 . The cancer therapeutic of claim 14 wherein the water-soluble copolymers comprise N-(2-hydroxypropyl) methacrylamide copolymers.
16 . The cancer therapeutic of claim 9 comprising a pharmaceutical composition.
17 . The cancer therapeutic of claim 16 comprising physiologically acceptable formulation agents.
18 . The cancer therapeutic of claim 16 wherein said cancer therapeutic is delivered intravenously.
19 . The cancer therapeutic of claim 16 wherein said cancer therapeutic is delivered orally.
20 . The cancer therapeutic of claim 16 comprising a combination therapeutic.
21 . The cancer therapeutic of claim 20 wherein the components of the combination therapeutic are delivered at the same time.
22 . The cancer therapeutic of claim 20 wherein the components of the combination therapeutic are delivered at different times.
23 . The cancer therapeutic of claim 20 wherein the components of the combination therapeutic are delivered intravenously.
24 . The cancer therapeutic of claim 20 wherein the components of the combination therapeutic are delivered orally.
25 . The cancer therapeutic of claim 20 wherein the components of the combination therapeutic are delivered by different methods.
26 . A method for treating cancer comprising the administration of a therapeutically effective amount of an enone selected from the following group, stereoisomers thereof, and positional isomers thereof
wherein X is a nucleophilic atom selected from the group consisting of S, N, and O and R is selected from the group consisting of OCOCH=CHCH 3 , OCOCH 3 , OCOC 6 H 5 , OCONHCH 3 , estrogen, testosterone, sex hormone steroids, and therapeutically active derivatives of sex hormone steroids.
27 . The enone of claim 26 comprising a derived glutathione adduct.
28 . The derived glutathione adduct of claim 26 wherein said glutathione adduct is produced by the action of glutathionyl transferase.
29 . The method of claim 26 wherein the therapeutically effective derivatives of sex hormone steroids comprise estradiol conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
30 . The method of claim 26 wherein the therapeutically effective derivatives of sex hormone steroids comprise testosterone conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
15 R′ = H, R =
16 R′ = H, R =
17 R = H, R′ =
18 R = H, R′ =
31 . The method of claim 26 wherein the enone comprises a polymeric substance in which the enone is bound to water-soluble copolymers.
32 . The method of claim 31 wherein the water-soluble copolymers comprise N-(2-hydroxypropyl) methacrylamide copolymers.
33 . The method of claim 26 wherein the enone comprises a physiologically acceptable pharmaceutical formulation.
34 . The method of claim 33 wherein the mode of delivery of the enone is intravenous.
35 . The method of claim 33 wherein the mode of delivery of the enone is oral.
36 . The method of claim 33 wherein the enone is delivered as part of a combination cancer therapeutic.
37 . The method of claim 36 wherein the components of the combination cancer therapeutic are delivered at the same time.
38 . The method of claim 36 wherein the components of the combination cancer therapeutic are delivered at different times.
39 . The method of claim 36 wherein the components of the combination cancer therapeutic are delivered intravenously.
40 . The method of claim 36 wherein the components of the combination cancer therapeutic are delivered orally.
41 . The method of claim 36 wherein the components of the combination cancer therapeutic are delivered by different methods.
42 . A method of making a glutathione adduct comprising:
a) selecting an enone from the following group, stereoisomers thereof, and positional isomers thereof wherein X is a nucleophilic atom selected from the group consisting of S, N, and O and R is selected from the group consisting of OCOCH=CHCH 3 , OCOCH 3 , OCOC 6 H 5 , OCONHCH 3 , estrogen, testosterone, sex hormone steroids, and therapeutically effective derivatives of sex hormone steroids; and b) reacting said enone with glutathionyl transferase.
43 . The method of claim 42 wherein the therapeutically effective derivatives of sex hormone steroids comprise estradiol conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
44 . The enone of claim 42 wherein the therapeutically effective derivatives of sex hormone steroids comprise testosterone conjugates selected from the following group, stereoisomers thereof, and positional isomers thereof
15 R′ = H, R =
16 R′ = H, R =
17 R = H, R′ =
18 R = H, R′ =
45 . The enone of claim 42 comprising a polymeric substance wherein the enone is bound to water-soluble copolymers.
46 . The enone of claim 45 wherein the water-soluble copolymers comprise N-(2-hydroxypropyl) methacrylamide copolymers.
47 . A method of treating cancer comprising:
a) delivering reactive compounds conjugated to tumor-targeting moieties into an individual; b) allowing said reactive compounds conjugated to tumor-targeting moieties to be transformed intracellularly by the nucleophilic addition of reduced glutathione; and c) allowing said transformed reactive compounds to then have their therapeutic effect by reacting, in turn, with cancer cell proteins or nucleic acids.Join the waitlist — get patent alerts
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